Family-wide Structural Analysis of Human Numb-Associated Protein Kinases

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Family-wide Structural Analysis of Human Numb-Associated Protein Kinases

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作者：Fiona J. Sorrell¹ ; Marta Szklarz¹ ; Kamal R. Abdul Azeez¹ ; Jon M. Elkins¹ ; Stefan Knapp¹ ; ² ; ^{knapp@pharmchem.uni-frankfurt.de" class="auth_mail" title="E-mail the corresponding author}
关键词：Numb-associated kinase (NAK) ; AAK1 ; BIKE ; inhibitor selectivity ; activation segment
刊名：Structure
出版年：2016
出版时间：1 March 2016
年：2016
卷：24
期：3
页码：401-411
全文大小：3334 K

文摘

•: First crystal structures of AAK1 and BIKE solved, completing the NAK family
•: Structural analysis of NAKs performed, revealing unusual family architecture
•: 144 clinical kinase inhibitors screened against AAK1, BIKE, GAK, and MPSK1
•: Nanomolar and covalent inhibitors discovered from clinical kinase library

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